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Literature summary for 3.4.21.75 extracted from

  • Feliciangeli, S.F.; Thomas, L.; Scott, G.K.; Subbian, E.; Hung, C.H.; Molloy, S.S.; Jean, F.; Shinde, U.; Thomas, G.
    Identification of a pH sensor in the furin propeptide that regulates enzyme activation (2006), J. Biol. Chem., 281, 16108-16116.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.75

Activating Compound

Activating Compound Comment Organism Structure
additional information His69 controls the pH-sensitive furin propeptide cleavage and enzyme activation in vitro. Protonated His69 disrupts the propeptide to expose the internal cleavage site and increases the efficiency of cleavage at Arg75 to yield the active enzyme Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
full-length epitope-tagged furin constructs or mutants expressed in A7 cells or BSC-40 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
H66L profurin mutant, shows no measurable effect on propeptide excision relative to the control (65% mature furin). No effect on the pH-triggered activation and propeptide release or on the trypsin-mediated unmasking of furin Homo sapiens
H69K profurin mutant, 80% reduced efficiency of propeptide excision, fails to be activated by acidic pH or trypsinolysis Homo sapiens
H69L profurin mutant, 70% reduced efficiency of propeptide excision. Completely blocked ability of acid pH to trigger furin activation and propeptide cleavage but shows no effect on the trypsin-mediated activation step. Propeptide fails to dissociate from mature furin Homo sapiens
R75A profurin mutant, substitution at the P1 position of the internal cleavage site, which blocks profurin activation but not propeptide excision or endoplasmic reticulum export of the furin-propeptide complex. No effect on the folding of the catalytic domain but blocked sensitivity of the furin-propeptide complex to acid pH Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
alpha1-antitrypsin
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum furin-propeptide complex is restricted to the endoplasmic reticulum by a PACS-2- and COPI-dependent mechanism. His69 is a pH sensor that allows enzyme activation following transport of the furin-propeptide complex from the endoplasmic reticulum to the mildly acidic TGN/endosomal system Homo sapiens 5783
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-RVKRGLAY(NO2)D-OH + H2O
-
 Homo sapiens ?
-
 ?